On November 2, 2006, Caroff, Eva; Fretz, Heinz; Hilpert, Kurt; Houille, Olivier; Hubler, Francis; Meyer, Emmanuel published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of N-(4-pyrimidinylcarbonyl) amino acid piperazides and their use as P2Y12 receptor antagonists. And the patent contained the following:
The invention relates to the preparation of title compounds I [R1 = (un)substituted Ph; W = a bond and R2 = CN, halo/alkoxy/heterocyclyl/cyclo/cycloalkyl/alkyl, hetero/ary/, heterocyclyl, (partially) saturated heterocyclyl; (un)substituted hydroxyalkyl; W = CH2 and R2 = NR7R8, SR9, SO2R10; W = O, S, and R2 = alkoxycarbonyl/carboxy/hydroxy/alkoxy/heterocyclyl/cyclo/ar/heteroaryl/alkyl, hetero/aryl; W = NH and derivatives and R2 = H, dialkylamino/alkoxycarbonyl/hydroxy/alkoxy/cyclo/heterocyclyl/cycloalkyl/ar/diphenyl/heteroaryl/alkyl, aryl, 2-phenylcyclopropyl, COR11, SO2R12, (un)substituted carboxyalkyl; W = CH:CH and R2 = hydroxy/alkoxy/alkyl alkoxycarbonyl, Ph, or CONR13R14; ; or W = CC and R2 = H, hydroxy/alkoxy/alkyl; or W = CO and R2 = alkyl; W = NR3 and NR2R3 = 4-7 membered heterocyclyl; or W = NR3 and NR2R3 = (un)substituted imidazoyl, pyrazolyl, 1,2,3-triazolyl, etc.; R5a, R5b = independently H, Me; R3 = H, alkyl; R7 aryl/alkyl; or NR7R8 = (un)substituted 4-7 membered heterocyclyl; R9 = cycloalkyl, aryl; R10 = cyclo/alkyl, aryl; R11 = alkoxy/alkyl, hetero/aryl, etc.; R12 = alkyl, aryl; R13, R14 = independently alkyl; X = CO and R6 = cyclo/alkyl, alk(ynyl)oxy, aryloxy, aralkoxy, hetero/aryl,aralkyl or NH2 and derivatives; or X = SO2 and R6 = alkyl; Y = a bond and Z = H, aryl substituted by carboxyalkoxy; or Y = alkoxy/Ph/alkoxyphenyl/alkylene, alkoxyphenylene and Z = H, OH, NH2, CO2H, tetrazolyl, CONH2, COOR17, NHCOR17, NHSO2R17; R17 = alkyl], as P2Y12 receptor antagonists. The invention also relates to the use of pyrimidines I and their stereoisomers, salts, solvent complexes and morphol. forms, in the treatment and/or prevention of peripheral vascular, visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases (no data) or conditions associated with platelet aggregation (no data), particularly thrombosis (no data). Thus, a multi-step synthesis starting from Z-L-Glu(Ot-Bu)-OH (Z = benzyloxycarbonyl) and 1-ethoxycarbonylpiperazine was given for amino acid piperazide II. In a P2Y12 binding assay, II had an IC50 = 117 nM. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Category: esters-buliding-blocks
The Article related to amino acid piperazide preparation p2y12 receptor antagonist thrombosis, platelet aggregation pyrimidinylcarbonyl amino acid piperazide preparation, piperazino carbonylmethylaminocarbonylpyrimidine preparation p2y12 antagonist and other aspects.Category: esters-buliding-blocks
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics